IL256423B - Crystalline fumarate salt of (s (-[4,3-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)] [3-hydroxy-3-(piperidin-2-yl)aztidine-1-yl]-methanone - Google Patents

Crystalline fumarate salt of (s (-[4,3-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)] [3-hydroxy-3-(piperidin-2-yl)aztidine-1-yl]-methanone

Info

Publication number: IL256423B
Authority: IL; Israel
Prior art keywords: fumarate salt; crystalline fumarate; crystalline; hydroxy; phenyl
Prior art date: 2015-06-30

Application number

IL256423A

Other languages

English (en)

Hebrew (he)

Other versions

IL256423A (en

Original Assignee

Exelixis Inc

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2015-06-30

Filing date

2016-06-30

Publication date

2022-09-01

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=56411938&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL256423(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2016-06-30 Application filed by Exelixis Inc filed Critical Exelixis Inc

2018-02-28 Publication of IL256423A publication Critical patent/IL256423A/en

2022-09-01 Publication of IL256423B publication Critical patent/IL256423B/en

Links

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Epidemiology (AREA)
Oncology (AREA)
Hematology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Hydrogenated Pyridines (AREA)
Plural Heterocyclic Compounds (AREA)

IL256423A 2015-06-30 2016-06-30 Crystalline fumarate salt of (s (-[4,3-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)] [3-hydroxy-3-(piperidin-2-yl)aztidine-1-yl]-methanone IL256423B (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US201562187009P	2015-06-30	2015-06-30
PCT/US2016/040444 WO2017004393A1 (en)	2015-06-30	2016-06-30	Crystalline fumarate salt of (s)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl) azetidin-1-yl]-methanone

Publications (2)

Publication Number	Publication Date
IL256423A IL256423A (en)	2018-02-28
IL256423B true IL256423B (en)	2022-09-01

Family

ID=56411938

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
IL256423A IL256423B (en)	2015-06-30	2016-06-30	Crystalline fumarate salt of (s (-[4,3-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)] [3-hydroxy-3-(piperidin-2-yl)aztidine-1-yl]-methanone
IL295052A IL295052A (en)	2015-06-30	2016-06-30	Crystalline fumarate salt of (s)-[4,3-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl)aztidine-1-yl]-methanone

Family Applications After (1)

Application Number	Title	Priority Date	Filing Date
IL295052A IL295052A (en)	2015-06-30	2016-06-30	Crystalline fumarate salt of (s)-[4,3-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl)aztidine-1-yl]-methanone

Country Status (35)

Country	Link
US (3)	US10590102B2 (sr)
EP (1)	EP3317264B1 (sr)
JP (3)	JP7338950B2 (sr)
KR (1)	KR102695324B1 (sr)
CN (2)	CN107810183A (sr)
AR (1)	AR105483A1 (sr)
AU (2)	AU2016288209B2 (sr)
CA (1)	CA2990222C (sr)
CL (1)	CL2017003475A1 (sr)
CO (1)	CO2018000086A2 (sr)
CR (1)	CR20180056A (sr)
DK (1)	DK3317264T3 (sr)
ES (1)	ES3058194T3 (sr)
FI (1)	FI3317264T3 (sr)
HK (1)	HK1252433A1 (sr)
HR (1)	HRP20251507T1 (sr)
IL (2)	IL256423B (sr)
LT (1)	LT3317264T (sr)
MA (1)	MA42301B1 (sr)
MD (1)	MD3317264T2 (sr)
MX (1)	MX390250B (sr)
MY (1)	MY192545A (sr)
PE (1)	PE20180692A1 (sr)
PH (1)	PH12017502414A1 (sr)
PL (1)	PL3317264T3 (sr)
PT (1)	PT3317264T (sr)
RS (1)	RS67509B1 (sr)
RU (2)	RU2762181C2 (sr)
SG (1)	SG10202105196YA (sr)
SI (1)	SI3317264T1 (sr)
SM (1)	SMT202500458T1 (sr)
TW (2)	TWI775187B (sr)
UA (1)	UA124728C2 (sr)
WO (1)	WO2017004393A1 (sr)
ZA (1)	ZA201708760B (sr)

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Publication number	Priority date	Publication date	Assignee	Title
KR102204520B1 (ko)	2012-10-12	2021-01-20	엑셀리시스, 인코포레이티드	암의 치료에 사용하기 위한 화합물의 신규 제조 방법
AR105483A1 (es)	2015-06-30	2017-10-11	Exelixis Inc	Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona
SI3881833T1 (sl) *	2015-06-30	2024-03-29	Genentech, Inc.,	Tablete s takojšnjim sproščanjem, ki vsebujejo zdravilo in postopek za oblikovanje tablet
ES2928773T3 (es)	2017-01-17	2022-11-22	Heparegenix Gmbh	Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos
GB201717809D0 (en) *	2017-10-30	2017-12-13	Azad Pharmaceutical Ingredients Ag	Process for the production of cobimetinib
WO2020187674A1 (en)	2019-03-15	2020-09-24	Sandoz Ag	Crystalline (s)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl][3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl]methanone hemisuccinate
WO2024111001A1 (en) *	2022-11-25	2024-05-30	Msn Laboratories Private Limited, R&D Center	Crystalline forms of n-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide fumarate and process for its preparation

Citations (1)

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Publication number	Priority date	Publication date	Assignee	Title
WO2008076415A1 (en) *	2006-12-14	2008-06-26	Exelixis, Inc.	Methods of using mek inhibitors

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ZA200703912B (en)	2004-10-20	2008-09-25	Serono Lab	3-arylamino pyridine derivatives
BRPI0611375A2 (pt)	2005-05-23	2010-08-31	Novartis Ag	formas cristalinas e outras de sais de ácido láctico de 4-amino-5-flúor-3-[6-(4-metilpiperazin-1-il)-1h-benzimid azol-2-il]-1h-quinolin-2-ona
SI1934174T1 (sl)	2005-10-07	2011-08-31	Exelixis Inc	Inhibitorji MEK in postopki za njihovo uporabo
CN101528231A (zh)	2006-08-16	2009-09-09	埃克塞利希斯股份有限公司	在癌症的治疗中使用pi3k和mek调控剂
WO2008124085A2 (en)	2007-04-03	2008-10-16	Exelixis, Inc.	Methods of using combinations of mek and jak-2 inhibitors
KR102204520B1 (ko)	2012-10-12	2021-01-20	엑셀리시스, 인코포레이티드	암의 치료에 사용하기 위한 화합물의 신규 제조 방법
CN105163584B (zh)	2013-03-05	2019-06-04	田纳西大学研究基金会	用于治疗癌症的化合物
MX2015010854A (es)	2013-03-14	2016-07-20	Genentech Inc	Combinaciones de un compuesto inhibidor de mek con un compuesto inhibidor de her3/egfr y metodos de uso.
AR105483A1 (es)	2015-06-30	2017-10-11	Exelixis Inc	Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona

2016
- 2016-06-24 AR ARP160101900A patent/AR105483A1/es unknown
- 2016-06-30 PL PL16738971.7T patent/PL3317264T3/pl unknown
- 2016-06-30 WO PCT/US2016/040444 patent/WO2017004393A1/en not_active Ceased
- 2016-06-30 MD MDE20180480T patent/MD3317264T2/ro unknown
- 2016-06-30 JP JP2017568050A patent/JP7338950B2/ja active Active
- 2016-06-30 MX MX2017017037A patent/MX390250B/es unknown
- 2016-06-30 IL IL256423A patent/IL256423B/en unknown
- 2016-06-30 FI FIEP16738971.7T patent/FI3317264T3/fi active
- 2016-06-30 MA MA42301A patent/MA42301B1/fr unknown
- 2016-06-30 CR CR20180056A patent/CR20180056A/es unknown
- 2016-06-30 UA UAA201800769A patent/UA124728C2/uk unknown
- 2016-06-30 CN CN201680039354.4A patent/CN107810183A/zh active Pending
- 2016-06-30 MY MYPI2017001962A patent/MY192545A/en unknown
- 2016-06-30 RU RU2018103172A patent/RU2762181C2/ru active
- 2016-06-30 SG SG10202105196YA patent/SG10202105196YA/en unknown
- 2016-06-30 LT LTEPPCT/US2016/040444T patent/LT3317264T/lt unknown
- 2016-06-30 TW TW109136325A patent/TWI775187B/zh active
- 2016-06-30 DK DK16738971.7T patent/DK3317264T3/da active
- 2016-06-30 AU AU2016288209A patent/AU2016288209B2/en active Active
- 2016-06-30 TW TW105120825A patent/TWI710556B/zh active
- 2016-06-30 CA CA2990222A patent/CA2990222C/en active Active
- 2016-06-30 SM SM20250458T patent/SMT202500458T1/it unknown
- 2016-06-30 SI SI201631936T patent/SI3317264T1/sl unknown
- 2016-06-30 RS RS20251247A patent/RS67509B1/sr unknown
- 2016-06-30 KR KR1020187000067A patent/KR102695324B1/ko active Active
- 2016-06-30 PT PT167389717T patent/PT3317264T/pt unknown
- 2016-06-30 PE PE2017002869A patent/PE20180692A1/es unknown
- 2016-06-30 CN CN202410400619.5A patent/CN118290395A/zh active Pending
- 2016-06-30 IL IL295052A patent/IL295052A/en unknown
- 2016-06-30 HK HK18111734.8A patent/HK1252433A1/zh unknown
- 2016-06-30 HR HRP20251507TT patent/HRP20251507T1/hr unknown
- 2016-06-30 EP EP16738971.7A patent/EP3317264B1/en active Active
- 2016-06-30 ES ES16738971T patent/ES3058194T3/es active Active
- 2016-06-30 RU RU2021132394A patent/RU2021132394A/ru unknown
2017
- 2017-12-21 ZA ZA2017/08760A patent/ZA201708760B/en unknown
- 2017-12-22 US US15/852,280 patent/US10590102B2/en active Active
- 2017-12-22 PH PH12017502414A patent/PH12017502414A1/en unknown
- 2017-12-29 CL CL2017003475A patent/CL2017003475A1/es unknown
2018
- 2018-01-05 CO CONC2018/0000086A patent/CO2018000086A2/es unknown
2020
- 2020-01-17 US US16/746,161 patent/US11254649B2/en active Active
- 2020-11-05 JP JP2020184868A patent/JP2021035967A/ja not_active Withdrawn
2021
- 2021-01-14 AU AU2021200202A patent/AU2021200202B2/en active Active
- 2021-11-08 US US17/521,396 patent/US20220056010A1/en not_active Abandoned
2022
- 2022-11-07 JP JP2022178184A patent/JP2023025000A/ja active Pending

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Also Published As

Publication number	Publication date
CL2017003475A1 (es)	2018-07-13
UA124728C2 (uk)	2021-11-10
NZ739160A (en)	2024-10-25
JP2018519318A (ja)	2018-07-19
SG10202105196YA (en)	2021-06-29
HK1252433A1 (zh)	2019-05-24
RU2021132394A (ru)	2021-11-18
MA42301B1 (fr)	2025-12-31
MA42301A (fr)	2018-05-09
FI3317264T3 (fi)	2025-12-05
US20200255398A1 (en)	2020-08-13
CA2990222A1 (en)	2017-01-05
CN118290395A (zh)	2024-07-05
MX390250B (es)	2025-03-20
CA2990222C (en)	2023-09-26
CO2018000086A2 (es)	2018-04-10
TW201718535A (zh)	2017-06-01
PL3317264T3 (pl)	2026-02-16
IL295052A (en)	2022-09-01
AR105483A1 (es)	2017-10-11
TW202108568A (zh)	2021-03-01
NZ777527A (en)	2024-10-25
JP2023025000A (ja)	2023-02-21
MX2017017037A (es)	2018-04-30
SI3317264T1 (sl)	2026-01-30
JP2021035967A (ja)	2021-03-04
ZA201708760B (en)	2022-06-29
US11254649B2 (en)	2022-02-22
KR102695324B1 (ko)	2024-08-13
TWI710556B (zh)	2020-11-21
PE20180692A1 (es)	2018-04-23
US20180346442A1 (en)	2018-12-06
AU2021200202A1 (en)	2021-03-18
PH12017502414A1 (en)	2018-06-25
EP3317264B1 (en)	2025-09-10
MY192545A (en)	2022-08-26
RS67509B1 (sr)	2025-12-31
US10590102B2 (en)	2020-03-17
KR20180021775A (ko)	2018-03-05
CN107810183A (zh)	2018-03-16
IL256423A (en)	2018-02-28
ES3058194T3 (en)	2026-03-09
WO2017004393A1 (en)	2017-01-05
PT3317264T (pt)	2025-12-12
TWI775187B (zh)	2022-08-21
HRP20251507T1 (hr)	2026-01-02
EP3317264A1 (en)	2018-05-09
JP7338950B2 (ja)	2023-09-05
DK3317264T3 (da)	2025-12-01
RU2018103172A3 (sr)	2019-10-31
AU2016288209A1 (en)	2018-02-08
RU2018103172A (ru)	2019-07-31
MD3317264T2 (ro)	2026-01-31
AU2016288209B2 (en)	2020-10-22
RU2762181C2 (ru)	2021-12-16
SMT202500458T1 (it)	2026-01-12
LT3317264T (lt)	2025-12-29
CR20180056A (es)	2018-05-25
BR112017028516A2 (pt)	2018-08-28
AU2021200202B2 (en)	2022-09-08
US20220056010A1 (en)	2022-02-24

Publication	Publication Date	Title
AU2021200202B2 (en)	2022-09-08	Crystalline fumarate salt of (s)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl) azetidin-1-yl]-methanone
JP6110817B2 (ja)	2017-04-05	大環状キナーゼ阻害剤の固体形態
EP3183252A1 (en)	2017-06-28	Oxalate salt of ruxolitinib
EP4027999B1 (en)	2026-03-04	Crystalline form of a multi-tyrosine kinase inhibitor, method of preparation, and use thereof
JP2023531078A (ja)	2023-07-20	化合物の結晶形態
HK40112789A (zh)	2025-01-28	结晶反丁烯二酸盐
KR20260044269A (ko)	2026-04-01	헌팅턴병 치료를 위한 스플라이싱 조절제인 6-(6-(((1r,2r,3s,5s)-2-플루오로-9-아자바이시클로[3.3.1]노난-3-일)(메틸)아미노)피리다진-3-일)-2-메틸벤조[d]옥사졸-5-올의 결정질 형태
BR112017028516B1 (pt)	2023-08-01	Sal de fumarato cristalino, seu uso, processo de preparação do mesmo e composição farmacêutica
WO2025164706A1 (ja)	2025-08-07	含窒素飽和複素環誘導体の結晶
IL324898A (en)	2026-01-01	New solid forms of (3r)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinozolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide